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TGR5-mediated bile acid sensing controls glucose homeostasis.
Targeting bile-acid signalling for metabolic diseases
- C. Thomas, R. Pellicciari, M. Pruzanski, J. Auwerx, K. Schoonjans
- Biology, MedicineNature Reviews Drug Discovery
- 1 August 2008
How the signalling functions of bile acids can be exploited in the development of drugs for obesity, type 2 diabetes, hypertriglyceridaemia and atherosclerosis, as well as other associated chronic diseases such as non-alcoholic steatohepatitis are reviewed.
Manipulation of Brain Kynurenines: Glial Targets, Neuronal Effects, and Clinical Opportunities
- R. Schwarcz, R. Pellicciari
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 October 2002
Pharmacological agents targeting specific KP enzymes can be used to normalize KP defects, show remarkable efficacy in animal models of central nervous system disorders, and offer novel therapeutic opportunities.
Family-wide chemical profiling and structural analysis of PARP and tankyrase inhibitors
Evaluated small-molecule inhibitors of poly-ADP-ribose polymerase (PARP) family proteins showed that the majority of PARP inhibitors bind multiple targets, providing insight into the design of new inhibitors.
6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.
6alpha-ethyl-chenodeoxycholic acid (6-ECDCA) was shown to be a very potent and selective FXR agonist and to be endowed with anticholeretic activity in an in vivo rat model of cholestasis.
The nuclear receptor SHP mediates inhibition of hepatic stellate cells by FXR and protects against liver fibrosis.
It is established that FXR ligands might represent a novel therapeutic option to treat liver fibrosis and that SHP binds JunD and inhibits DNA binding of adaptor protein (AP)-1 induced by thrombin.
Structural basis for bile acid binding and activation of the nuclear receptor FXR.
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.
- Hiroyuki Sato, A. Macchiarulo, J. Auwerx
- Biology, ChemistryJournal of medicinal chemistry
- 29 February 2008
The biological screening of a collection of natural occurring bile acids, bile acid derivatives, and some steroid hormones has resulted in the discovery of new potent and selective T GR5 ligands and a binary classification model of TGR5 activity is developed.
TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading.
Pharmacological characterization of 1-aminoindan-1,5-dicarboxylic acid, a potent mGluR1 antagonist.
- F. Moroni, G. Lombardi, R. Pellicciari
- Biology, ChemistryThe Journal of pharmacology and experimental…
- 1 May 1997
The pharmacological profile of 1-aminoindan-1,5-dicarboxylic acid, a rigid (carboxyphenyl)glycine derivative acting on metabotropic glutamate receptors (mGluRs) is examined to suggest that AIDA is a potent, selective and competitive mGluR1 a antagonist.